A comprehensive review of diclofenac pharmacology

June 30, 2025

Oana Andreia Coman 1, Ruxandra-Cristina Marin 1 *, Laurentiu Coman 2, Mihnea Costescu 1, Ion Fulga 1

1 Department of Pharmacology, Clinical Pharmacology and Pharmacotherapy, Faculty of Medicine, Carol Davila University of Medicine and Pharmacy, Bucharest, Romania
2 Medical Center for Diagnosis, Outpatient Treatment and Preventive Medicine, Bucharest, Romania
* Correspondence to: Ruxandra-Cristina Marin, Department of Pharmacology, Clinical Pharmacology and Pharmacotherapy, Faculty of Medicine, Carol Davila University of Medicine and Pharmacy, 050474 Bucharest, Romania. E-mail: rcfhm@yahoo.com

Abstract

Diclofenac, the standard comparator for many studies that aim to evaluate the efficacy and safety of other non-steroidal anti-inflammatory molecules, is one of the most used drugs of its class due to its good efficacy versus safety profile. This article is a review of the most important information regarding the pharmaceutic, pharmacokinetic and pharmacodynamic properties, therapeutic indications and contraindications of diclofenac. A special attention is addressed to the oral and topical pharmaceutical forms that are the most comfortable and accepted by patients, consequently, the most used. The innovation in manufacturing technologies led to the emergence of new pharmaceutical forms that generated major changes in the pharmacokinetics of the active substance and, consequently, in its pharmacodynamics, mainly by increasing efficiency in rheumatic diseases. Thus, the innovative pharmaceutical forms of diclofenac bring about an improvement of some pharmacokinetic characteristics and parameters such as bioavailability following administration on different routes, preferential distribution at the site of action, faster elimination from plasma, along with long-term maintenance of active and effective concentrations in target tissues (synovia, muscles etc.). Finally, all these advances in pharmaceutical formulation increase therapeutic efficacy, treatment adherence and significantly reduce the risk of adverse reactions.